(S)-4-(苯基甲基)-2-吗啉甲醇 | 132073-82-6

• 物质功能分类: 医药中间体 - 杂环化合物
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (S)-4-(苯基甲基)-2-吗啉甲醇
• 中文别名: (S)-(4-苄基吗啉-2-基)甲醇
• 英文名称: (S)-(4-benzylmorpholin-2-yl)methanol
• 英文别名: (S)-4-Benzyl-2-(hydroxymethyl)morpholine；[(2S)-4-benzylmorpholin-2-yl]methanol
• CAS: 132073-82-6
• 化学式: C₁₂H₁₇NO₂
• 分子量: 207.272
• InChiKey: WQNIKIMRIXHNFF-LBPRGKRZSA-N

物化性质

• 沸点：
  303.2±27.0 °C(Predicted)
• 密度：
  1.117±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302

反应信息

• 作为反应物：
  描述：

  (S)-4-(苯基甲基)-2-吗啉甲醇 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 12.0h， 以99%的产率得到(S)-吗啉-2-甲醇
  参考文献：
  名称：

  Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors

  摘要：

  合成了一系列取代有吗啉-嘧啶衍生物的吡嗪-3-酮，并评估其作为c-Met酶的酪氨酸激酶抑制剂以及对Hs746T人胃癌细胞系的抗增殖活性。大多数化合物表现出良好的生物活性，其中化合物10、12a和14a展现了优异的c-Met酶抑制活性和Hs746T细胞基础活性。

  DOI：

  10.1007/s12272-015-0703-7
• 作为产物：
  描述：

  在 盐酸 、 lithium aluminium tetrahydride 、 sodium ethanolate 、 三乙胺 作用下， 以 四氢呋喃 、 乙醇 、 丁酮 为溶剂， 反应 86.0h， 生成 (S)-4-(苯基甲基)-2-吗啉甲醇
  参考文献：
  名称：

  Yanagisawa, Hiroaki; Kanazaki, Takuro, Heterocycles, 1993, vol. 35, # 1, p. 105 - 109

  摘要：

  DOI：

文献信息

• 신규한 히드라진온이 치환된 피리미딘 유도체 및 그의 용도
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY 한국화학연구원(319980077651)

  公开号：KR101842645B1

  公开（公告）日：2018-03-29

  본 발명은 신규한 히드라진온이 치환된 피리미딘 유도체 또는 이의 약제학적 허용 가능한 염, 이들을 유효성분으로 포함하는 c-Met 티로신 키나아제 활성 억제용 약제학적 조성물 및 이상증식성 질환(hyper proliferative disorder)의 예방 또는 치료용 약제학적 조성물에 관한 것이다. 본 발명은 c-Met 티로신 키나아제의 활성을 효율적으로 억제함으로써 비정상적인 키나제의 활성으로 인한 과도한 세포 증식 및 성장과 관련된 다양한 이상증식성 질환, 예를 들어 암, 건선, 류마티스 관절염, 당뇨병성 망막증 등의 치료제로 유용하게 이용될 수 있다.

  本发明涉及一种新型的已替代的嘧啶衍生物或其药学上可接受的盐，包括这些作为有效成分的用于抑制c-Met酪氨酸激酶活性的药学组合物，以及用于预防或治疗增生性疾病的药学组合物。本发明通过有效地抑制c-Met酪氨酸激酶的活性，可以将其用作治疗与异常激酶活性相关的过度细胞增殖和生长的各种增生性疾病，例如癌症、银屑病、类风湿性关节炎、糖尿病性视网膜病变等。
• Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors
  作者：Eun-Young Kim、Seung-Tae Kang、Heejung Jung、Chi Hoon Park、Chang-Soo Yun、Jong Yeon Hwang、Byung Jin Byun、Chong Ock Lee、Hyoung Rae Kim、Jae Du Ha、Do Hyun Ryu、Sung Yun Cho

  DOI：10.1007/s12272-015-0703-7

  日期：2016.4

  A series of pyridazin-3-one substituted with morpholino-pyrimidine derivatives was synthesized and evaluated as tyrosine kinase inhibitors against c-Met enzyme, and anti-proliferative activities of Hs746T human gastric cancer cell line. Most of compounds exhibited good biological activity, while compound 10, 12a, 14a displayed excellent c-Met enzyme inhibitory activities and Hs746T cell-based activities.

  合成了一系列取代有吗啉-嘧啶衍生物的吡嗪-3-酮，并评估其作为c-Met酶的酪氨酸激酶抑制剂以及对Hs746T人胃癌细胞系的抗增殖活性。大多数化合物表现出良好的生物活性，其中化合物10、12a和14a展现了优异的c-Met酶抑制活性和Hs746T细胞基础活性。
• [EN] MORPHOLINO COMPOUNDS, USES AND METHODS<br/>[FR] COMPOSÉS MORPHOLINO, UTILISATIONS ET PROCÉDÉS
  申请人：UNIV DUNDEE

  公开号：WO2012160392A1

  公开（公告）日：2012-11-29

  The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.

  该发明涉及根据式（I）的吗啡啉衍生物或其立体异构体或药用可接受的盐或溶剂化物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、m和n如规范中定义。这些化合物是G蛋白偶联受体的拮抗剂、逆向激动剂或激动剂，例如多巴胺D4和5HT1a。该发明还涉及包括这些化合物的药物组合物和涉及这些化合物和组合物的方法。该发明的化合物和组合物特别可用于治疗疾病和疾病，如神经和神经退行性疾病；或作为设计和选择更多治疗化合物的引导化合物。
• MORPHOLINO COMPOUNDS, USES AND METHODS
  申请人：University of Dundee

  公开号：US20140148452A1

  公开（公告）日：2014-05-29

  The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.

  该发明涉及按照式(I)的吗啡啉衍生物或其立体异构体或药用可接受的盐或溶剂，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、m和n如规范中定义。这些化合物是G蛋白偶联受体的拮抗剂、反向激动剂或激动剂，例如多巴胺D4和5HT1a。该发明还涉及包括这些化合物的药物组合物和涉及这些化合物和组合物的方法。该发明的化合物和组合物特别可用于治疗疾病和障碍，如神经系统和神经退行性疾病；或作为设计和选择进一步治疗化合物的引导化合物。
• NOVEL TRIAZOLOPYRAZINE DERIVATIVE AND USE THEREOF
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：US20150259350A1

  公开（公告）日：2015-09-17

  The present invention relates to a novel triazolopyrazine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating hyper proliferative disorder. The present invention can be useful as a therapeutic agent for various hyper proliferative disorders associated with excessive cell proliferation and growth caused by abnormal kinase activity, such as cancer, psoriasis, rheumatoid arthritis, and diabetic retinopathy, by efficiently inhibiting c-Met tyrosine kinase activity.

  本发明涉及一种新型三唑吡嗪衍生物或其药用盐，以及含有该衍生物作为活性成分的药物组合物，用于预防或治疗过度增殖性疾病。本发明可以作为治疗剂，用于有效抑制c-Met酪氨酸激酶活性，从而对抗与异常激酶活性引起的细胞过度增殖和生长相关的各种过度增殖性疾病，如癌症、银屑病、类风湿性关节炎和糖尿病视网膜病变。